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20-September-2008 09:55:47 - Calcium channel blocker November 2007 Calcium channel blockers are a class of drugs and natural substances with effects on many excitable cells of the body, like the muscle of the heart, smooth muscles of the vessels or neuron cells. The latter are used as antiepileptics and are not covered in this article. The main action of calcium channel blockers is to decrease the blood pressure. It is for this action that it is used in individuals with hypertension. Contents 1 Explanation 2 Mechanism of action 3 Classes of calcium channel blockers 3.1 Dihydropyridine 3.2 Phenylalkylamine 3.3 Benzothiazepine 4 Other drugs with similar uses 5 See also 6 External links Explanation Most calcium channel blockers decrease the force of contraction of the myocardium muscle of the heart. This is known as the negative inotropic effect of calcium channel blockers. It is because of the negative inotropic effects of most calcium channel blockers that they are avoided or used with caution in individuals with cardiomyopathy. Many calcium channel blockers also slow down the conduction of electrical activity within the heart, by blocking the calcium channel during the plateau phase of the action potential of the heart see: cardiac action potential. This is known as a negative dromotropic effect. It causes a lowering of the heart rate and may cause heart blocks, which is known as the negative chronotropic effect of calcium channel blockers. The negative chronotropic effects of calcium channel blockers make them a commonly used class of agents in individuals with atrial fibrillation or flutter in whom control of the heart rate is an issue. Mechanism of action Calcium channel blockers work by blocking voltage-gated calcium channels VGCCs in muscle cells of the heart and blood vessels. This prevents calcium levels from increasing as much in the cells when stimulated, leading to less muscle contraction. In the heart, a decrease in calcium available for each beat results in a decrease in cardiac contractility. In blood vessels, a decrease in calcium results in less contraction of the vascular smooth muscle and therefore an increase in blood vessel diameter, a phenomenon called vasodilation. Vasodilation decreases total peripheral resistance, while a decrease in cardiac contractility decreases cardiac output. Since blood pressure is in part determined by cardiac output and peripheral resistance, blood pressure drops. With a relatively low blood pressure, the afterload on the heart decreases; this decreases the amount of oxygen required by the heart. This can help ameliorate symptoms of ischemic heart disease such as angina pectoris. Unlike β-blockers, calcium channel blockers do not decrease the responsiveness of the heart to input from the sympathetic nervous system. Since moment-to-moment blood pressure regulation is carried out by the sympathetic nervous system via the baroreceptor reflex, calcium channel blockers allow blood pressure to be maintained more effectively than do β-blockers. However, because calcium channel blockers result in a decrease in blood pressure, the baroreceptor reflex often initiates a reflexive increase in sympathetic activity leading to increased heart rate and contractility. A β-blocker may be combined with a calcium channel blocker to minimize these effects. Ionic calcium is antagonized by magnesium ions in the nervous system. Because of this, dietary supplements of magnesium oxide and other magnesium preparations may increase or enhance the effects of calcium channel blockade. 1 Classes of calcium channel blockers Dihydropyridine Dihydropyridine calcium channel blockers are often used to reduce systemic vascular resistance and arterial pressure, but are not used to treat angina with the exception of amlodipine, which carries an indication to treat chronic stable angina as well as vasospastic angina because the vasodilation and hypotension can lead to reflex tachycardia. This CCB class is easily identified by the suffix -dipine. Amlodipine Norvasc Aranidipine Sapresta Azelnidipine Calblock Barnidipine HypoCa Benidipine Coniel Cilnidipine Atelec, Cinalong, Siscard Clevidipine Cleviprex Efonidipine Landel Felodipine Plendil Lacidipine Motens, Lacipil Lercanidipine Zanidip Manidipine Calslot, Madipine Nicardipine Cardene, Carden SR Nifedipine Procardia, Adalat Nilvadipine Nivadil Nimodipine Nimotop Nisoldipine Baymycard, Sular, Syscor Nitrendipine Cardif, Nitrepin, Baylotensin Pranidipine Acalas Side effects of these synthetic drugs may include but are not limited to: Dizziness, headache, redness in the face Fluid buildup in the legs Rapid heart rate. Slow heart rate. Constipation Gingival overgrowth Phenylalkylamine Skeletal formula of verapamil Skeletal formula of verapamil Phenylalkylamine calcium channel blockers are relatively selective for myocardium, reduce myocardial oxygen demand and reverse coronary vasospasm, and are often used to treat angina. They have minimal vasodilatory effects compared with dihydropyridines. Action is intracellular. Verapamil Calan, Isoptin Gallopamil Procorum, D600 Benzothiazepine Structural formula of diltiazem Structural formula of diltiazem Benzothiazepine calcium channel blockers are an intermediate class between phenylalkylamine and dihydropyridines in their selectivity for vascular calcium channels. By having both cardiac depressant and vasodilator actions, benzothiazepines are able to reduce arterial pressure without producing the same degree of reflex cardiac stimulation caused by dihydropyridines. Diltiazem Cardizem Other drugs with similar uses Other classes of pharmaceutical agents that have overlapping effects as calcium channel blockers include ACE inhibitors, beta-blockers, and nitrates. See also Voltage-dependent calcium channel External links MeSH Calcium+Channel+Blockers Official Adalat Nifedipine site, Bayer Video - Calcium Channel Blockers v d e Calcium channel blockers C08 Dihydropyridines Amlodipine Aranidipine Azelnidipine Barnidipine Benidipine Cilnidipine Clevidipine Efonidipine Felodipine Isradipine Lacidipine Manidipine Lercanidipine Nicardipine Nifedipine Nilvadipine Nimodipine Nisoldipine Nitrendipine Pranidipine Phenylalkylamines Gallopamil Verapamil Benzothiazepines Diltiazem Others Naftopidil v d e Medications used in the management of pulmonary arterial hypertension B01, C02 Prostacyclin analogues Beraprost, Epoprostenol, Iloprost, Treprostinil Endothelin receptor antagonists Ambrisentan, Bosentan, Sitaxsentan PDE5 inhibitors Sildenafil, Tadalafil Adjunctive therapy Calcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin v d e Antiarrhythmic agents C01B class I Na+ channel blockers class Ia Phase 0 Ajmaline Disopyramide Prajmaline Procainamide Quinidine Sparteine class Ib Phase 3 Aprindine Lidocaine Mexiletine Tocainide class Ic Phase 0 Encainide Flecainide Lorcainide Moricizine Propafenone class II Phase 4, beta blockers Propranolol Metoprolol Nadolol Atenolol Acebutolol Pindolol class III Phase 3, K+ channel blockers Amiodarone Bretylium tosylate Bunaftine Dofetilide Ibutilide Nifekalant Sotalol class IV Phase 4, Ca2+ channel blockers Verapamil Diltiazem class V other A1 agonist Adenosine muscarinic antagonist Atropine cardiac glycoside Digoxin Retrieved from http://en..org/wiki/Calcium_channel_blocker Categories: Calcium channel blockersHidden categories: Articles lacking sources from November 2007 | All articles lacking sources Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages العربية Deutsch Español Ù?ارسی Français Italiano Nederlands 日本語 Polski Português РуÑ?Ñ?кий Svenska ไทย This page was last modified on 17 August 2008, at 15:21
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